C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 309/30 (2006.01) C07D 307/33 (2006.01)
Patent
CA 2634749
A process is provided for the preparation of a key intermediate in the preparation of 2'-branched nucleoside compounds. The process includes contacting a protected precursor 3,4-O-isopropylidene-2-C- substituted-D-arabinono-1,5-lactone with a fluorinating agent under anhydrous conditions and converting the precursor into a protected 2-deoxy-2-halo-2-C-disubstituted ribono-1,5-lactone and optionally into a 2- deoxy-2-halo-2-C-disubstituted ribono- 1,4-lactone.
L'invention concerne un procédé pour la préparation d'un intermédiaire important pour la préparation de composés nucléosides ramifiés en 2'. Le procédé consiste à faire entrer en contact un précurseur 3,4-O-isopropylidène-2-C-substitué-D-arabinono-l,5-lactone protégé avec un agent fluoré dans des conditions anhydres et à convertir le précurseur en une 2-déoxy-2-halo-2-C-disubstitué ribono-l,5-lactone protégée et facultativement une 2- déoxy-2-halo-2-C-disubstitué ribono- 1 ,4-lactone.
Mayes Benjamin Alexander
Moussa Adel
Idenix Pharmaceuticals Inc.
Osler Hoskin & Harcourt Llp
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